Details of the Drug Formulation (DFM)

General Information of DFM (ID: F23750)
Name
Fluocinonide 0.1% cream
Company
Perrigo New York
Active Pharmaceutical Ingredient (API) Fluocinonide API Info click to show the detail info of this API
Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E09QIG DIG Info Citric acid monohydrate Acidulant ...
E03GBZ DIG Info Diisopropanolamine Buffering agent ...
E06WYP DIG Info Glycerin Antimicrobial preservative ...
E0H2RX DIG Info Glyceryl monostearate Emollient ...
E0BG2A DIG Info Isostearic acid Emulsifying agent ...
E0M1JK DIG Info Propylene glycol Antimicrobial preservative ...
E0H2SC DIG Info Water Solvent
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      G-protein coupled receptor (GPCR)
            DBT Name: Olfactory receptor 51E2 (OR51E2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Isostearic acid
                    Biological Activity EC50 = 9.8 nM (estimated based on the structural similarity with CHEMBL82293 ) [1]
                    Structural Similarity Tanimoto coefficient = 0.886363636
                    Tested Species Homo sapiens (Human)
                    UniProt ID O51E2_HUMAN
      Oxidoreductase (ORase)
            DBT Name: Albendazole monooxygenase (CYP3A4) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Propylene glycol
                    Biological Activity Inhibition ratio < 20 % (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
      Primary active transporter (PAT)
            DBT Name: Multidrug resistance protein 2 (ABCC2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Glyceryl monostearate
                    Biological Activity Inhibition ratio = 76 % (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MRP2_HUMAN
            DBT Name: Multidrug resistance protein 1 (ABCB1) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Glyceryl monostearate
                    Biological Activity Protein expression downregulation = 52.3 % (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Glyceryl monostearate
                    Biological Activity Inhibition ratio = 46 % (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Glyceryl monostearate
                    Biological Activity Inhibition ratio = 47 % (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
      Other protein families (OPF)
            DBT Name: Epidermal lipid-binding protein (E-FABP) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Isostearic acid
                    Biological Activity IC50 = 1200 nM (estimated based on the structural similarity with CHEMBL82293 ) [5]
                    Structural Similarity Tanimoto coefficient = 0.886363636
                    Tested Species Homo sapiens (Human)
                    UniProt ID FABP5_HUMAN
      Cell line (CELL)
            DBT Name: Leukemia L1210 cells (L1210) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Diisopropanolamine
                    Biological Activity IC50 = 600 nM (estimated based on the structural similarity with CHEMBL77102 ) [6]
                    Structural Similarity Tanimoto coefficient = 0.860465116
                    Tested Species Mus musculus (Mouse)
                    Cellosaurus ID CVCL_0382
            DBT Name: Prostate cancer LNCaP cells (LNCaP) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Glyceryl monostearate
                    Biological Activity IC50 > 100000 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0395
            DBT Name: Lymphoma S49 cells (S49) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Isostearic acid
                    Biological Activity EC50 = 500000 nM (estimated based on the structural similarity with CHEMBL82293 ) [8]
                    Structural Similarity Tanimoto coefficient = 0.886363636
                    Tested Species Mus musculus (Mouse)
                    Cellosaurus ID CVCL_D198
References
1 US patent application no. 20180116992A1, Modulators of Prostate-Specific G-Protein Receptor (PSGR/OR51E2) and Methods of Using Same.
2 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
3 Effects of monoglycerides on rhodamine 123 accumulation, estradiol 17 beta-D-glucuronide bidirectional transport and MRP2 protein expression within Caco-2 cells. J Pharm Pharm Sci. 2008;11(3):45-62.
4 Effects of monoglycerides on P-glycoprotein: modulation of the activity and expression in Caco-2 cell monolayers. Mol Pharm. Sep-Oct 2008;5(5):863-75.
5 Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target. Bioorg Med Chem Lett. 2004 Sep 6; 14(17):4445-8.
6 Synthesis and evaluation of hydroxylated polyamine analogues as antiproliferatives. J Med Chem. 2001 Jul 19; 44(15):2451-9.
7 Lignanamides and nonalkaloidal components of Hyoscyamus niger seeds. J Nat Prod. 2002 Feb; 65(2):206-9.
8 2'-O-Acyl-6-thioinosine cyclic 3',5'-phosphates as prodrugs of thioinosinic acid. J Med Chem. 1979 Jul; 22(7):811-5.

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